Interaction of articaine hydrochloride with prokaryotic membrane lipids.
OBJECTIVE
Local anesthetics are the most commonly used drugs in dentistry, with a wide range of effects, including antimicrobial activity. High antimicrobial effects have recently been reported on oral microbes from articaine hydrochloride, revealed by the minimum inhibitory concentration and minimal bactericidal concentration. Additionally, articaine has recently been used as an alkaline component in endodontic materials with a proposed antibacterial activity. However, the detailed mechanisms of action have not been discussed.


METHODS
We determined the Langmuir surface pressure/molecular area isotherms of prokaryotic lipid monolayers, as well as the phospholipid phase transitions, by employing differential scanning calorimetry on unilamellar prokaryotic liposomes (bilayers).


RESULTS
Articaine hydrochloride was found to interact with the prokaryotic membrane lipids in both monolayers and bilayers. An increase of the phospholipid molecular area of acidic glycerophospholipids as well as a decrease in phase transition temperature and enthalpy were found with increasing articaine hydrochloride concentration. The thermodynamic changes by adding articaine hydrochloride to prokaryotic membrane lipids are potentially related to the effects observed from antimicrobial peptides resulting from membrane insertion, aggregate composition, pore formation, and lysis.


CONCLUSIONS
Interaction of articaine hydrochloride with prokaryotic membrane lipids is indicated. Hence, further research is necessary to gain insight into where these compounds exert their effects at the molecular level.
Lygre
Henning
H
Department of Medicine, Section of Pharmacology, University of Bergen, Bergen, Norway. henning.lygre@med.uib.no
Moe
Grete
G
Nerdal
Willy
W
Holmsen
Holm
H
D000766:Anesthesia, Dental; D000779:Anesthetics, Local / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002355:Carticaine / Q000737:chemistry*; D002462:Cell Membrane / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D008081:Liposomes; D008563:Membrane Lipids / Q000737:chemistry*; D044367:Phase Transition; D010743:Phospholipids / Q000737:chemistry*; D011387:Prokaryotic Cells; D044366:Transition Temperature
D000779:Anesthetics, Local; D000900:Anti-Bacterial Agents; D008081:Liposomes; D008563:Membrane Lipids; D010743:Phospholipids; D002355:Carticaine